Catalog No.S3032 Synonyms: AF 2838
Molecular Weight(MW): 324.37
Bindarit exhibits selective inhibition against monocyte chemotactic proteins MCP-1/CCL2, MCP-3/CCL7 and MCP-2/CCL8.
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Differential participation of ATRs or MCP-1/CCR2 signaling in RVLM in pressor response and tachycardia after stroke. Changes in mean diastolic (ΔDBP) blood pressure or heart rate (ΔHR) relative to baseline in rats that received pretreatment by microinjection bilaterally into the RVLM of bindarit (Bin; 10 nmol, MCP-1 synthesis inhibitor), BMS CCR2 22 (BMS; 10 pmol, CCR2 antagonist), propagermanium (Prop; 10 pmol, CCR2 antagonist) or vehicle control (Veh).Values are mean ± SEM, n = 5-7 animals per experimental group. *P < 0.05 versus SC group, and +P < 0.05 versus Veh (Saline) + MCAO group in the post hoc Scheffe multiple-range test.
Neurobiol Dis 2014 71, 292-304. Bindarit purchased from Selleck.
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|Description||Bindarit exhibits selective inhibition against monocyte chemotactic proteins MCP-1/CCL2, MCP-3/CCL7 and MCP-2/CCL8.|
|Features||Bindarit is devoid of immunosuppressive effects.|
Bindarit treatment causes a dose-dependent inhibition of the capacity of human monocytes to produce monocyte chemotactic protein-1 (MCP-1) in response to bacterial LPS or C. albicans with IC50 of 172 µM and 403 µM, respectively. The inhibition of LP-induced MCP-1 production by Bindarit is associated with reduced levels of MCP-1 mRNA transcripts with IC50 of 75 µM. Bindarit inhibits the production of MCP-1 by LPS-stimulated MM6 cells with IC50 of 425 μM, without affecting the release of IL-8 or IL-6.  Bindarit treatment inhibits the release of MCP-1 from IL-1 stimulated osteoblast cell line Saos-2.  Bindarit, even at the maximal concentration, does not exhibit a direct in vitro cytotoxic effect on human IIB-MEL-J melanoma or ECs, although it inhibits MCP-1 expression.  Bindarit (10-300 μM) reduces rat vascular smooth muscle cell (VSMC) proliferation, migration, and invasion.  Bindarit induces the downregulation of the classical NF-κB pathway. Bindarit displays a specific inhibitory effect on the p65 and p65/p50 induced MCP-1 promoter activation, with no effect on other tested activated promoters, indicating that Bindarit acts on a specific subpopulation of NF-κB isoforms and selects its targets within the whole NF-κB inflammatory pathway.  Bindarit modulates cancer-cell proliferation and migration, mainly through negative regulation of TGF-β and AKT signaling. 
|In vivo||Oral administration of Bindarit at 50 mg/kg in NZB/W mice delays the onset of proteinuria, significantly protects from renal function impairment, and prolongs survival of NZB/W mice or lupus mice. Bindarit treatment completely MCP-1 up-regulation during the progression of nephritis.  Inhibition of MCP-1 with Bindarit also reduces tumor growth and macrophage recruitment, rendering necrotic tumor masses in human melanoma xenografts.  Bindarit is effective in reducing neointima formation in both non-hyperlipidaemic and hyperlipidaemic animal models of vascular injury by a direct effect on VSMC proliferation and migration and by reducing neointimal macrophage content.  Administration of Bindarit results in impaired metastatic disease in prostate cancer PC-3M-Luc2 xenograft mice and impairment of local tumorigenesis in Balb/c mice with murine breast cancer 4T1-Luc cells. In addition, Bindarit treatment significantly decreases the infiltration of tumor-associated macrophages and myeloid-derived suppressor cells in 4T1-Luc primary tumors. |
-  Zoja C, et al. Kidney Int, 1998, 53(3), 726-734.
-  Sironi M, et al. Eur Cytokine Netw, 1999, 10(3), 437-442.
-  Guglielmotti A, et al. Inflamm Res, 2002, 51(5), 252-258.
|In vitro||DMSO||64 mg/mL (197.3 mM)|
|Ethanol||64 mg/mL (197.3 mM)|
|In vivo||Add solvents individually and in order:
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT01269242||Completed||Coronary Restenosis||Aziende Chimiche Riunite Angelini Francesco S.p.A||January 2009||Phase 2|
|NCT01109212||Completed||Diabetic Nephropathy||Aziende Chimiche Riunite Angelini Francesco S.p.A|Mario Negri Institute for Pharmacological Research||March 2007||Phase 2|
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